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The crystal structure of the B subtilis Maf BSU
2019-09-24
The crystal structure of the B. subtilis Maf (BSU28050) was published in 2000, and, to date, it represents the only experimental work with a purified Maf protein (Minasov et al., 2000). The structure revealed a structural fold similar to that found in ITPases and YjjX proteins, which are nucleotide
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The mechanisms by which coregulators control the actions of
2019-09-23
The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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CYP A and CYP D are
2019-09-23
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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br Acknowledgments br Multicellular organisms respond
2019-09-23
Acknowledgments Multicellular organisms respond rapidly, and adapt to cellular stress to maximize cell survival. The cellular stress response, also called (ISR), is universally conserved and independent of the stressor. ISR induces rapid, transient reprogramming of cellular protein translation
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br Cytokine impact on ILC fate Increasing evidence
2019-09-23
Cytokine impact on ILC fate Increasing evidence shows that ILC2 and ILC3 may convert into ILC1-like Rosiglitazone by downregulating either GATA3 or RORγt, respectively, upregulating T-bet and gaining the capacity for IFN-γ production [60,61]. This process, often referred to as ‘ILC plasticity’, m
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br Author Contributions br Acknowledgments br Introduction
2019-09-23
Author Contributions Acknowledgments Introduction Osteoporosis is a common bone disease that frequently leads to disruption of the alveolar and systemic bones with age. Novel osteoanabolic strategies to treat osteoporotic bone loss or augment fracture repair efficiently are desired. Since b
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Two parameters were extracted from these
2019-09-23
Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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Structural homology modelling Intensive Phyre modelling was
2019-09-23
Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino BI-D1870 sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E. coli adenine-N6-
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DNA damage represents a persistent threat to genomic stabili
2019-09-23
DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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br Cysteine proteases as molecular targets for
2019-09-23
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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Materials and methods Cell culture and receptor gene transfe
2019-09-23
Materials and methods Cell culture and receptor gene transfection. PC12 inhibitor review were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifted by
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A cocktail approach can detect the activities of
2019-09-23
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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Apart from its high affinity the selection of
2019-09-23
Apart from its high affinity, the selection of GW2580 as fda approved lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehen
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The pharmacokinetics properties of compound
2019-09-23
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability
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In summary our findings indicate
2019-09-23
In summary, our findings indicate that bFGF stimulates CPT1 expression, FA oxidation and lactate production with the participation of PPARβ/δ activation. On the other hand, this investigation shows that FSH concomitantly regulates the expression of genes involved in FA metabolism and in mitochondria
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